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目的设计合成3-取代苯甲酰基-4H-色烯-4-酮类化合物,并测定其体外抗快速增殖分枝杆菌活性。方法以焦性没食子酸和取代苯甲酸为原料,经Friedel-Crafts酰基化、Baker-Venkataraman重排等反应合成目标化合物,初步测定了目标化合物的抗快速增殖分枝杆菌活性。结果共合成8个3-取代苯甲酰基-4H-色烯-4-酮类化合物,其结构经核磁共振氢谱和质谱确证。化合物2a、2e呈现边缘抗快速增殖分枝杆菌活性。结论在具有抗快速增殖分枝杆菌活性的天然产物(S)-3-(4-甲氧苄基)-7,8-亚甲二氧基二氢高异黄酮的2,3-位引入双键、7,8-位更换为甲氧基以及9位以羰基替代亚甲基均会导致抗快速增殖分枝杆菌活性的大幅降低。
OBJECTIVE To design and synthesize 3-substituted benzoyl-4H-chromen-4-ones and determine their in vitro activities against Mycobacterium fastae. Methods The target compounds were prepared by Friedel-Crafts acylation and Baker-Venkataraman rearrangement using pyrogallol and substituted benzoic acids as starting materials. The activity of the target compounds against Mycobacterium fast-proliferati was determined preliminarily. Results A total of 8 3-substituted benzoyl-4H-chromen-4-ones were synthesized and their structures were confirmed by 1H NMR and MS. Compounds 2a, 2e exhibited edge anti-fast Mycobacterium proliferative activity. Conclusions Bis (4-methoxybenzyl) -7,8-methylenedioxydiphosphate is introduced into the 2,3-position of the natural product (S) -3- Bond, the substitution of the 7,8-position for the methoxy group and the substitution of the carbonyl group for the 9-position to the methylene group led to a substantial reduction in the activity against Mycobacterium fast-proliferati on.